Abstract: Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.

Abstract: A process for the large-scale chemoenzymatic production of (6S)-5-methyl-5,6,7,8-tetrahydrofolic acid, also known as (6S)-5-methylTHFA, the process comprising the steps of: (1) reducing folic acid (FA) so as to yield dihydrofolic acid (DHFA); (2) stereoselectively reducing DHFA with dihydrofolate reductase (DHFR) in the presence of NADP/NADPH, glucose and GluDH so as to yield (6S)-THFA; (3) converting (6S)-THFA to (6S)-5-methlTHFA; and (4) isolating (6S)-5-methylTHFA.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and an ?-(methanesulfonyl)alkenylnitrile compound, or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering an ?-(methanesulfonyl)alkenylnitrile compound or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof. Oral and topical administration are preferred.

Abstract: The present invention relates to processes for preparing 3-methylsulfonylpropionitrile. The processes provide a good yield and a good purity of the final product and provide a controllable reaction. The present invention also relates to a crystalline form of 3-methylsulfonylpropionitrile having X-ray diffraction peaks at 13.9±0.1, 19.2±0.1, 20.0±0.1, 22.5±0.1, 23.2±0.1, 25.7±0.1, 28.1±0.1, 29.9±0.1, and 30.6±0.1 degrees 2?, and wherein the most intense peak is the peak at 13.9±0.1 degrees 2?.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and ?-(methylsulfonyl)alkylamine or ?-(methylsulfonyl)alkylamide. The present invention is also directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering ?-(methylsulfonyl)alkylamine or ?-(methylsulfonyl)alkylamide, or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and 3-(methylthio)propionitrile, or a pharmaceutically acceptable salt thereof. The present invention is directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering ?-(methylthio)alkylnitriles such as 3-(methylthio)propionitrile, or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a ?-(arylsulfonyl)alkylnitrile compound, or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering an ?-(arylsulfonyl)alkylnitrile compound or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and diethyl(2-cyanoethyl)phosphonate, or a pharmaceutically acceptable salt thereof. The present invention is directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering diethyl(2-cyanoethyl)phosphonate, or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: The present invention provides a novel approach for the preparation of fatty alcohol esters of ?-hydroxy carboxylic acids. In one form of the invention, the target fatty alcohol ester of ?-hydroxy carboxylic acid is produced by converting a lower alkyl ester of ?-hydroxy carboxylic acid into a fatty alcohol ester of ?-hydroxy carboxylic acid via alcoholysis (i.e., transesterification). The transesterification process is an equilibrium reaction, catalyzed chemically (i.e., with acids or bases) or enzymatically, that is shifted in the desired direction to produce the desired product. One way of shifting the reaction in the direction of the desired product is by reducing the concentration of one of the products (e.g., distillation of a lower-boiling alcohol as it is formed). Another preferred way of shifting the reaction in the direction of the desired product is by increasing the concentration of one of the reactants.

Abstract: Described herein are compositions (e.g., a pharmaceutical composition) and methods for controlling the delivery of a therapeutic agent, and their use in the treatment and/or prevention of diseases and disorders.

Abstract: The present invention relates to processes for preparing 3-methylsulfonylpropionitrile. The processes provide a good yield and a good purity of the final product and provide a controllable reaction. The present invention also relates to a crystalline form of 3-methylsulfonylpropionitrile having X-ray diffraction peaks at 13.9±0.1, 19.2±0.1, 20.0±0.1, 22.5±0.1, 23.2±0.1, 25.7±0.1, 28.1±0.1, 29.9±0.1, and 30.6±0.1 degrees 2?, and wherein the most intense peak is the peak at 13.9±0.1 degrees 2?.

Abstract: The present invention relates to processes for preparing 3-methylsulfonylpropionitrile. The processes provide a good yield and a good purity of the final product and provide a controllable reaction. The present invention also relates to a crystalline form of 3-methylsulfonylpropionitrile having X-ray diffraction peaks at 13.9±0.1, 19.2±0.1, 20.0±0.1, 22.5±0.1, 23.2±0.1, 25.7±0.1, 28.1±0.1, 29.9±0.1, and 30.6±0.1 degrees 2?, and wherein the most intense peak is the peak at 13.9±0.1 degrees 2?.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a methanesulfonylalkylnitrile compound, or a pharmaceutically acceptable salt or solvate thereof. The present invention is also directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering a methanesulfonylalkylnitrile compound or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a ?-(arylsulfonyl)alkylnitrile compound, or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering an ?-(arylsulfonyl)alkylnitrile compound or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: Described herein are compositions (e.g., a pharmaceutical composition) and compounds of formula I, methods of making compounds of formula (I) and their use in the treatment and/or prevention of diseases and disorders.

Abstract: Described herein are compositions (e.g., a pharmaceutical composition) and compounds of formula I, and their use in the treatment and/or prevention of diseases and disorders.

Abstract: Described herein are compositions (e.g., a pharmaceutical composition) and methods for controlling the delivery of a therapeutic agent, and their use in the treatment and/or prevention of diseases and disorders.

Abstract: A process for the large-scale chemoenzymatic production of (6S)-5-methyl-5,6,7,8-tetrahydrofolic acid, also known as (6S)-5-methylTHFA, the process comprising the steps of: (1) reducing folic acid (FA) so as to yield dihydrofolic acid (DHFA); (2) stereoselectively reducing DHFA with dihydrofolate reductase (DHFR) in the presence of NADP/NADPH, glucose and GluDH so as to yield (6S)-THFA; (3) converting (6S)-THFA to (6S)-5-methlTHFA; and (4) isolating (6S)-5-methylTHFA,

Abstract: The present invention provides a novel approach for the preparation of fatty alcohol esters of ?-hydroxy carboxylic acids. In one form of the invention, the target fatty alcohol ester of ?-hydroxy carboxylic acid is produced by converting a lower alkyl ester of ?-hydroxy carboxylic acid into a fatty alcohol ester of ?-hydroxy carboxylic acid via alcoholysis (i.e., transesterification). The transesterification process is an equilibrium reaction, catalyzed chemically (i.e., with acids or bases) or enzymatically, that is shifted in the desired direction to produce the desired product. One way of shifting the reaction in the direction of the desired product is by reducing the concentration of one of the products (e.g., distillation of a lower-boiling alcohol as it is formed). Another preferred way of shifting the reaction in the direction of the desired product is by increasing the concentration of one of the reactants.

Abstract: The present invention provides a novel approach for the preparation of fatty alcohol esters of ?-hydroxy carboxylic acids. In one form of the invention, the target fatty alcohol ester of ?-hydroxy carboxylic acid is produced by converting a lower alkyl ester of ?-hydroxy carboxylic acid into a fatty alcohol ester of ?-hydroxy carboxylic acid via alcoholysis (i.e., transesterification). The transesterification process is an equilibrium reaction, catalyzed chemically (i.e., with acids or bases) or enzymatically, that is shifted in the desired direction to produce the desired product. One preferred way of shifting the reaction in the direction of the desired product is by reducing the concentration of one of the products (e.g., distillation of a lower-boiling alcohol as soon as it is formed). Another preferred way of shifting the reaction in the direction of the desired product is by increasing the concentration of one of the reactants (e.g., adding more of the starting ester).